Tight junction regulator studied for celiac disease, leaky gut, and intestinal permeability research. Competitive inhibitor of zonulin — the protein that opens intestinal tight junctions. Phase 3 trials conducted for celiac.
Topically active in gut lumen; minimal systemic absorption by design
SKUs
1
Evidence
Moderate Evidence
Larazotide (also known as AT-1001) is a synthetic octapeptide that has been studied primarily for celiac disease. It works by reducing intestinal permeability — specifically targeting a protein called zonulin that regulates the tight junctions between intestinal cells. It is the first compound specifically designed to address the intestinal permeability aspect of celiac disease and has completed phase 2 and phase 3 trials.
Celiac Disease Research
Larazotide has been the primary focus of multiple clinical trials in celiac disease. Phase 2 trials showed reductions in intestinal permeability and improvements in GI symptoms in patients on a gluten-free diet who continued to have symptoms. Phase 3 trials examined it as an add-on to gluten-free diet.
Intestinal Permeability Research
Larazotide targets tight junction regulation, making it an important research tool for studying how zonulin and tight junction proteins govern intestinal barrier function. This research has implications beyond celiac disease for conditions associated with elevated intestinal permeability.
Gut Barrier Biology
Beyond celiac disease, some research has examined whether larazotide's mechanism of restoring tight junctions could be relevant for other conditions involving intestinal permeability, including inflammatory bowel disease and food sensitivities.
Phase 2 trials in celiac disease showed reductions in intestinal permeability markers.
GI symptom improvements observed in patients on gluten-free diet with persistent symptoms.
Phase 3 trial data have been analyzed and have not shown strong efficacy on primary endpoints.
The intestinal permeability mechanism is well-characterized and validated as a research approach.
The phase 3 trial for celiac disease did not meet primary endpoints, which is a significant limitation for this compound's development path. While mechanistically interesting, the clinical evidence for meaningful symptom benefit in celiac disease patients is not conclusive from the phase 3 data. It is not FDA-approved for any indication.
The lining of the small intestine is made up of cells joined together by protein structures called tight junctions — think of them as seals between individual tiles. In celiac disease and some other gut conditions, these seals can be disrupted by a protein called zonulin, which is triggered by gluten and other factors. When tight junctions open, the intestinal barrier becomes more permeable, allowing partially digested food particles and bacterial products to slip through into the bloodstream and trigger immune reactions. Larazotide is designed to block the receptor that zonulin uses to signal the tight junctions to open, essentially keeping the seals closed and preventing the intestinal barrier from being compromised after a gluten exposure.
Larazotide was generally well-tolerated in clinical trials, with a side effect profile comparable to placebo in most studies. GI symptoms were the most common adverse events. It is not FDA-approved. The phase 3 data are available and suggest it is safe, though its efficacy did not reach statistical significance on primary outcomes.
Moderate Evidence
This compound has been studied in Phase 1 or Phase 2 human trials. Evidence is encouraging but more large-scale trials are needed.
Published Research Ranges
0.5–2mg three times daily oral in celiac phase 2/3 trials
Research Context Only: These are ranges reported in published scientific studies for educational reference. They are not dosing recommendations. This is not medical advice. Always consult a qualified healthcare professional.
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Research Education Only: This profile is for educational purposes only. All information is sourced from published scientific literature. This is not medical advice. Not for human consumption. Consult qualified medical professionals for any health decisions.
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